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GSK1120212B

Phase 1

Cancer | Small molecule | Oncology |GSK plc|Trials Updated: Nov 13, 2017

GSK1120212B development status

Highest phase Phase 1
Registered trials 1 across 1 sponsor since Aug 2011

GSK1120212B target and mechanism

ModalitySmall molecule

Also known as GSK1120212B (Standard DMSO content)

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment80

FDA Designations

No designations recorded

GSK1120212B clinical trials

GSK1120212B · 1 trial · 1 indication

Phase 1 1
NCT01725100A Study to Determine the Relative Bioavailability of the MEK Inhibitor, Trametinib, in Subjects With Solid Tumor MalignanciesCancer
COMPLETED80 Analytics
PHASE1COMPLETED
A Study to Determine the Relative Bioavailability of the MEK Inhibitor, Trametinib, in Subjects With Solid Tumor Malignancies
CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Corrected Cmax of GSK1120212B
Period 1 and 2: Day 1 pre-dose within 15 minutes (mins) of planned study treatment administration (serves as the 168-hour [hr] sample for Period 1), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 10 hrs post-dose; Days 2 to 7: post dose at 24 hrs (Day 2), 48 hrs (

Pharmacokinetic data will include corrected maximum plasma concentration (Cmax) of GSK1120212B. Comparison of Cmax will enable to determine the relative bioavailability of the test formulation with lower DMSO content (Treatment B) and the standard reference formulation (Treatment A). Period 2 PK parameters will be corrected for residual concentrations from Period 1 (based on individual estimates of t1/2) to remove the carry-over effect.

Corrected AUC(0-t) and AUC(0-inf) of GSK1120212B
Period 1 and 2: Day 1 pre-dose within 15 mins of planned study treatment administration (serves as the 168-hr sample for Period 1), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 10 hrs post-dose; Days 2 to 7: post dose at 24 hrs (Day 2), 48 hrs (Day 3), 72 hrs (

Pharmacokinetic data will include corrected area under the time-concentration curve from time zero (pre-dose) to last time of quantifiable concentration (AUC(0-t)) and AUC from zero to infinity (AUC(0-inf)) of GSK1120212B. Period 2 PK parameters will be corrected for residual concentrations from Period 1 (based on individual estimates of t1/2) to remove the carry-over effect.

Corrected tmax of GSK1120212B
Period 1 and 2: Day 1 pre-dose within 15 mins of planned study treatment administration (serves as the 168-hr sample for Period 1), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 10 hrs post-dose; Days 2 to 7: post dose at 24 hrs (Day 2), 48 hrs (Day 3), 72 hrs (

Pharmacokinetic data will include corrected time of occurrence of Cmax (tmax) of GSK1120212B. Period 2 PK parameters will be corrected for residual concentrations from Period 1 (based on individual estimates of t1/2) to remove the carry-over effect.

Secondary Endpoints

Uncorrected Cmax of GSK1120212B
For Period 1 and 2 on Day 1: pre-dose within 15 mins of planned study treatment administration (serves as the 168-hr sample for Period 1), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 10 hrs post-dose; Days 2 to 7: post dose at 24 hrs (Day 2), 48 hrs (Day 3), 72
Uncorrected AUC(0-t), AUC(0-inf) and AUC(0-24) of GSK1120212B
For Period 1 and 2 on Day 1: pre-dose within 15 mins of planned study treatment administration (serves as the 168-hr sample for Period 1), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 10 hrs post-dose; Days 2 to 7: post dose at 24 hrs (Day 2), 48 hrs (Day 3), 72
Pre-dose concentration (C0) of GSK1120212B
Period 2: Day 1 pre-dose within 15 minutes (mins) of planned study treatment administration (serves as the 168-hour [hr] sample for Period 1.
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeOTHER

Treatment Arms

ArmTypeDescription
Treatment A: GSK1120212B (Standard DMSO content)EXPERIMENTALSubjects will receive Treatment A in Period 1 or 2 as single oral dose on Day 1 of Period 1 or 2 in fasting condition with water.
Treatment B: GSK1120212B (Lower DMSO content)EXPERIMENTALSubjects will receive Treatment B in Period 1 or 2 as single oral dose on Day 1 of Period 1 or 2 in fasting condition with water.

Interventions

NameTypeDescription
GSK1120212B (Standard DMSO content)DRUGEach tablet contains GSK1120212B equivalent to 2 mg of GSK1120212 as drug substance. The coated tablets have a standard DMSO content of theoretical 11.3%.
GSK1120212B (Lower DMSO content)DRUGEach tablet contains GSK1120212B equivalent to 2 mg of GSK1120212 as drug substance. The coated tablets have a lower DMSO content approximately 9.5%.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites4

Inclusion Criteria: * Has provided signed, written informed consent. * Male or female, age \>=18 years of age at the time of signing the informed consent form. * Has histologically or cytologically confirmed diagnosis of a solid tumor malignancy that is not responsive to standard therapy (ies) or f...

Countries:United States
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Competitive Landscape -Cancer 7 trials

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Frequently asked questions about GSK1120212B

What is GSK1120212B?

GSK1120212B is an investigational small molecule in Phase 1 development at GSK plc for cancer. It is a MEK inhibitor, studied in solid tumor malignancies. The compound has been evaluated in a single completed Phase 1 trial in the United States. It is not an approved therapy and remains in clinical development.

What does GSK1120212B target?

GSK1120212B targets MEK, a kinase in the MAPK signaling pathway. It is described as a MEK inhibitor. By targeting MEK, the drug is designed to interfere with signaling that drives tumor cell growth in solid tumors. The Phase 1 study of GSK1120212B was conducted in subjects with solid tumor malignancies.

Who makes GSK1120212B?

GSK1120212B is developed by GSK plc, which trades under the ticker GSK. The company sponsored the Phase 1 study of the compound in patients with solid tumor malignancies. GSK plc is the developer of record for this MEK inhibitor asset.

What phase is GSK1120212B in?

GSK1120212B is in Phase 1 development. It has been studied in one completed Phase 1 trial in cancer. The drug is investigational and has not been approved for any indication. No active trials of GSK1120212B are currently listed.

What clinical trials is GSK1120212B in?

GSK1120212B has been studied in one clinical trial, NCT01725100, titled A Study to Determine the Relative Bioavailability of the MEK Inhibitor, Trametinib, in Subjects With Solid Tumor Malignancies. That Phase 1 trial enrolled 80 participants in the United States and is completed. It was controlled and randomized, without double blinding.

Is GSK1120212B the same as GSK1120212B (Standard DMSO content)?

Yes. GSK1120212B is also known as GSK1120212B (Standard DMSO content). The parenthetical refers to the standard DMSO content form of the compound. Both names refer to the same investigational MEK inhibitor developed by GSK plc for cancer.